A phenol sandwich fights diabetes

被引：3

作者：

Bernardi, Anna ^{[1
]}

Sattin, Sara ^{[1
]}

机构：

[1] Univ Milan, Dept Chem, Milan, Italy

来源：

NATURE CHEMICAL BIOLOGY | 2015年 / 11卷 / 09期

关键词：

INHIBITORS; AMYLASE;

D O I：

10.1038/nchembio.1888

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

The complex flavonoid montbretin A (MbA) is a powerful inhibitor of human pancreatic amylase (HPA) and a potential tool in the treatment of type 2 diabetes. The X-ray structure of the MbA–HPA complex now shows that a hydrophobic collapse of two phenol fragments in the structure of MbA is key to its activity.

引用

页码：635 / 636

页数：3

共 8 条

[1]

Campo VL, 2013, SPR CARB CH, V39, P181, DOI 10.1039/9781849737173-00181

[2] Identification and Characterization of Acidic Mammalian Chitinase Inhibitors [J].

Cole, Derek C. ;

Olland, Andrea M. ;

Jacob, Jaison ;

Brooks, Jon ;

Bursavich, Matthew G. ;

Czerwinski, Robert ;

DeClereq, Charlene ;

Johnson, Mark ;

Joseph-McCarthy, Diane ;

Ellingboe, John W. ;

Lin, Laura ;

Nowak, Pawel ;

Presman, Ella ;

Strand, James ;

Tam, Amy ;

Williams, Cara M. M. ;

Yao, Shihua ;

Tsao, Desiree H. H. ;

Fitz, Lori J. .

JOURNAL OF MEDICINAL CHEMISTRY, 2010, 53 (16) :6122-6128

[3] Adherence to Therapies in Patients with Type 2 Diabetes [J].

Garcia-Perez, Luis-Emilio ;

Alvarez, Maria ;

Dilla, Tatiana ;

Gil-Guillen, Vicente ;

Orozco-Beltran, Domingo .

DIABETES THERAPY, 2013, 4 (02) :175-194

[4]

Gloster TM, 2012, NAT CHEM BIOL, V8, P683, DOI [10.1038/NCHEMBIO.1029, 10.1038/nchembio.1029]

[5] A Small Molecule That Inhibits OGT Activity in Cells [J].

Ortiz-Meoz, Rodrigo F. ;

Jiang, Jiaoyang ;

Lazarus, Michael B. ;

Orman, Marina ;

Janetzko, John ;

Fan, Chenguang ;

Duveau, Damien Y. ;

Tan, Zhi-Wei ;

Thomas, Craig J. ;

Walker, Suzanne .

ACS CHEMICAL BIOLOGY, 2015, 10 (06) :1392-1397

[6] The search for novel human pancreatic α-amylase inhibitors:: High-throughput screening of terrestrial and marine natural product extracts [J].

Tarling, Chris A. ;

Woods, Kate ;

Zhang, Ran ;

Brastianos, Harry C. ;

Brayer, Gary D. ;

Andersen, Raymond J. ;

Withers, Stephen G. .

CHEMBIOCHEM, 2008, 9 (03) :433-438

[7]

Williams LK, 2015, NAT CHEM BIOL, V11, P691, DOI [10.1038/NCHEMBIO.1865, 10.1038/nchembio.1865]

[8] Order and Disorder: Differential Structural Impacts of Myricetin and Ethyl Caffeate on Human Amylase, an Antidiabetic Target [J].

Williams, Leslie K. ;

Li, Chunmin ;

Withers, Stephen G. ;

Brayer, Gary D. .

JOURNAL OF MEDICINAL CHEMISTRY, 2012, 55 (22) :10177-10186

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